
Clonidine: Difference between revisions
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Binding affinities: | Binding affinities: | ||
* | Clonidine shows agonism at the following receptors, namely the alpha (α) receptors. It lowers blood pressure by stimulating the α<sub>2</sub> receptors in the brain. | ||
* | *α<sub>1A</sub> receptor: 316.23 nM | ||
* | *α<sub>1B</sub> receptor: 316.23 nM | ||
* | *α<sub>1D</sub> receptor: 125.89 nM | ||
* | *α<sub>2A</sub> receptor: 42.92 nM | ||
* | *α<sub>2B</sub> receptor: 106.31 nM | ||
*α<sub>2C</sub> receptor: 233.1 nM | |||
Clonidine also binds to the Imidazoline I<sub>1</sub> receptor as an agonist. | |||
==Subjective effects== | ==Subjective effects== | ||
{{EffectStub}} | {{EffectStub}} |
Revision as of 20:26, 12 July 2017
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Template:SubstanceBox/clonidine Clonidine (also known by the trade names Catapres, Kapvay, Nexiclon, Clophelin, and others) is a medication used to treat high blood pressure, attention deficit hyperactivity disorder, anxiety disorders, tic disorders, substance withdrawal (from either alcohol, opioids, or smoking tobacco), migraine, menopausal flushing, diarrhea, and certain pain conditions.[1] It is classified as a centrally acting α2 adrenergic agonist and imidazoline receptor agonist. It has been in clinical use for over 40 years.[2]
Chemistry
Clonidine is an imdiazoline compound, meaning that its main chemistry is of an imidazole ring. A nitrogen bonded to the imidazole and chlorinated phenyl group makes an amine.
Pharmacology
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This pharmacology section is incomplete. You can help by adding to it. |
Binding affinities: Clonidine shows agonism at the following receptors, namely the alpha (α) receptors. It lowers blood pressure by stimulating the α2 receptors in the brain.
- α1A receptor: 316.23 nM
- α1B receptor: 316.23 nM
- α1D receptor: 125.89 nM
- α2A receptor: 42.92 nM
- α2B receptor: 106.31 nM
- α2C receptor: 233.1 nM
Clonidine also binds to the Imidazoline I1 receptor as an agonist.
Subjective effects
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This subjective effects section is a stub. As such, it is still in progress and may contain incomplete or wrong information. You can help by expanding or correcting it. |
Toxicity and harm potential
It is strongly recommended that one use harm reduction practices when using this drug, especially concurrently with other depressants.
Lethal dosage
According to dailymed.nlm.nih.gov's prescribing information page for clonidine, clonidine's oral LD50 in mice is 206 mg/kg and for rats, 465 mg/kg. Of course, this does not mean one will not die with levels below these. The treatment for clonidine overdose is naloxone.
Tolerance and addiction potential
Clonidine seems to be able to cause addiction and can be tolerated over periods of time. It is used concurrently with prescription pain-killers (opioids) recreationally because it might have potentiating effects, but this has not been studied.
Legal issues
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This legality section is a stub. As such, it may contain incomplete or wrong information. You can help by expanding it. |
United States: In the US, clonidine is only available through prescription.
See also
References
- ↑ Brayfield, A, ed. (13 January 2014). "Clonidine". Martindale: The Complete Drug Reference. London, UK: Pharmaceutical Press. Retrieved 28 June 2014.
- ↑ Neil, MJ (November 2011). "Clonidine: clinical pharmacology and therapeutic use in pain management.". Current Clinical Pharmacology. 6 (4): 280–7. PMID 21827389.
https://pubchem.ncbi.nlm.nih.gov/compound/clonidine#section=Names-and-Identifiers http://onlinelibrary.wiley.com/doi/10.1002/ddr.430020207/full
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